Grünenthal’s proprietary NaV 1.8 inhibitor enters clinical development

The Phase I trial will involve 70 healthy volunteers and comprises a Single Ascending Dose and a Multiple Ascending Dose part. It aims to assess the safety and tolerability profile and the pharmacokinetic characteristics of the investigational medicine. In addition, the trial will generate initial insights into the compound’s pharmacology through a cold-pressor test.

“Inhibition of Na_V 1.8 offers an exciting opportunity to provide patients with urgently needed non-opioid pain therapies,” says Uli Brödl, Chief Scientific Officer, Grünenthal. “While we have seen the first medicine targeting Na_V 1.8 receive FDA approval last year, we are committed to driving further innovation in this field where advanced assets may provide enhanced patient outcomes by blocking Na_V 1.8 more comprehensively.”

About voltage-gated sodium channels (Na_V)

There are a total of nine different Na_V channels in the human body. The Na_V 1.8 channel is a clinically and genetically validated pain target, as the channel plays a significant role in triggering excitatory signals in nociceptive neurons, which the human brain perceives as pain. Blocking the Na_V 1.8 channel to suppress or prevent its excitatory signalling will provide a significant analgesic effect across a range of chronic and acute pain conditions.